Abstract

A cephalexin (CEP) self-nanoemulsifying drug delivery system (SNEDDS) was developed in this study to improve the drug’s oral administration. The CEP-SNEDDS was made utilizing an aqueous titration method employing Lauroglycol 90, Poloxamer 188, and Transcutol-HP. Box-Behnken design (BBD) with three factors at three levels was used for optimization, and their impacts on globule size (nm), transmittance (percent), and emulsification time (s) were assessed. The optimized formulation (Opt-F3) was further tested for zeta potential, refractive index, percent transmittance, thermodynamic stability, in-vitro release, ex vivo permeability, antibacterial activity, and bioavailability. The chosen formulation (Opt-F3) had a globule size of 87.25 ± 3.16 nm, PDI of 0.25, zeta potential of −24.37 mV, self-emulsification duration of 52 ± 1.7 s, and percentage transmittance of 99.13 ± 1.5%, viscosity of 96.26 ± 2.72 cp, and refractive index of 1.29 ± 0.1. It showed a sustained release profile (94.28 ± 5.92 percent in 24 h). The Opt-F3 formulation had 3.95 times the permeability of CEP-dispersion. In comparison to CEP-dispersion, it also demonstrated greater antibacterial efficacy against tested Gram-positive and Gram-negative pathogens. The oral bioavailability of Opt-F3 is 3.48 times higher than that of CEP-dispersion, according to an in-vivo investigation. It has been determined that the prepared CEP-SNEDDS may be an advantageous carrier for CEP delivery.

Highlights

  • Cephalexin (CEP) is a first-generation cephalosporin derivative that is given orally

  • It is listed as a key access antibiotic in the World Health Organization’s essential drug list and it is used as a second choice drug in the form of oral delivery for the effective treatment of chronic obstructive pulmonary disease (COPD), pharyngitis, skin, and soft tissue infections [4]

  • Cephalexin is a water-insoluble antibiotic with a half-life of 1 to 1.5 h [5]

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Summary

Introduction

Cephalexin (CEP) is a first-generation cephalosporin derivative that is given orally. It belongs to the β-lactam class of antibiotics and is commercially available as a monohydrate. It has chemical formula C16 H17 N3 O4 S·H2 O and a molecular weight of 365.41 g/mol [1]. It is effective in the treatment of Staphylococci and Streptococci infections [2]. Cephalexin is a water-insoluble antibiotic with a half-life of 1 to 1.5 h [5]. Maintaining therapeutic levels in the blood is critical for short-half-life antibiotics in order to avoid resistance [8,9]

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